Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/263)
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Patent number: 7148227Abstract: The invention relates to triazolopyrimidines of formula (I), in which the substituents are defined as follows: L1 represents cyano, S(?O)nA1 or C(?O)A2, wherein A1 stands for hydrogen, hydroxy, alkyl, alkylamino or dialkylamino; A2 stands for C1–C8 alkoxy, C1–C6 haloalkoxy or one of the groups named in A1; and n stands for 0, 1 or 2; L2, L3 represent hydrogen or halogen; L4, L5 represent hydrogen, halogen or alkyl; X represents halogen, cyano, alkyl, haloalkyl, alkoxy or haloalkoxy; R1 represents alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, alkadienyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, phenyl, naphthyl, or a five to ten-membered saturated, partially unsaturated or aromatic heterocyclus containing between one and four heteroatoms from the group containing O, N or S; R2 represents hydrogen or R1; R1 and R2 can form, together with the nitrogen atom to which they are bonded, a five or six-membered ring, which can be interrupted and/or substituted by an atom from the groupType: GrantFiled: March 19, 2003Date of Patent: December 12, 2006Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl, Ulrich Schöfl
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Patent number: 7105664Abstract: 5-Halogen-6-phenyl-7-fluoroalkylamino-triazolopyrimidines of formula I: (I) in which R1 is hydrogen, fluoro, alkyl, alkenyl, alkynyl, alkadienyl, where the carbon chains of these radicals may be unsubstituted or substituted as defined in the description; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, where these radicals may be unsubstituted or substituted; R3 is fluoroalkyl or fluoroalkenyl; X is halogen; n is 0 or an integer from 1 to 4; L each independently is halogen, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy. Processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.Type: GrantFiled: April 6, 2002Date of Patent: September 12, 2006Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Eberhard Ammermann, Klaus-Jürgen Pees, Guido Albert, Annerose Rehnig, Debra Search
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Patent number: 7094894Abstract: Disclosed are a method for producing fungicidal triazolopyrimidine compounds, agents containing said compounds, and the use thereof for controlling harmful fungi. Also disclosed are triazolopyrimidines of formula (I), in which the substituents have the following meaning: L1 represents alkyl; L2 represents halogen; L3represents hydrogen or halogen; X represents halogen, cyano, alkyl, alkoxy, or haloalkoxy; R1, R2 represent hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, alkadienyl, alkinyl, or cycloalkinyl, phenyl, naphthyl, or a five-unit to ten-unit saturated, partially unsaturated, or aromatic heterocycle containing one to four heteroatoms from the group O, N, or S, R1 and R2 can also form a five-unit or six-unit ring along with the nitrogen atom to which they are linked. Said ring can be interrupted and/or substituted by an atom from the group O, N, and S while R1 and/or R2 can be substituted according to the description.Type: GrantFiled: April 30, 2003Date of Patent: August 22, 2006Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7094782Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: November 7, 2003Date of Patent: August 22, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 7091209Abstract: A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and tautomers thereof, and pharmaceutically acceptable salts or esters thereof; and inhibitors of viral polymerases, especially the hepatitis C virus (HCV) polymerase enzymeType: GrantFiled: July 11, 2001Date of Patent: August 15, 2006Assignee: Merck & Co., Inc.Inventors: Cristina Gardelli, Claudio Giuliano, Steven Harper, Uwe Koch, Frank Narjes, Jesus Maria Ontoria Ontoria, Marco Poma, Simona Ponzi, Ian Stansfield, Vincenzo Summa
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Patent number: 7084146Abstract: The novel compounds of formula I: wherein R1 is hydrogen or methyl; R2 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl or phenyl group; Hal is halogen; and L1 through L5 are each hydrogen, halogen, alkyl, alkoxy or nitro, provided that at least one of L1 through L5 represents nitro or alkoxy; show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.Type: GrantFiled: April 23, 2001Date of Patent: August 1, 2006Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Guenter Krummel, Henry Van Tuyl Cotter, Guido Albert, Annerose Rehnig, Leslie May, Waldemar Pfrengle
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Patent number: 7071334Abstract: 6-(2-Chloro-6-fluoro-phenyl)-triazolopyrimidines of formula (I), in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, alkadienyl, or haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or partially or fully halogenated or may be substituted as defined in the description.Type: GrantFiled: April 6, 2002Date of Patent: July 4, 2006Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7067520Abstract: The present invention provides a preventive or therapeutic medicine for diabetes containing as an active ingredient a fused-heterocyclic compound of the formula (I?) or its salt: [wherein G is CN, NO2, CO2R4, CHO, SO2NRaRb or CONRaRb; R1 is a halogen atom, a —O—R5 group or a —S—R5 group; R2 is a halogen atom, a —O—R5 group (wherein R5 is as defined above) or an amino group which may be substituted; and each of R8 and R10 which are independent of each other, is a hydrogen atom, a halogen atom or an alkyl group].Type: GrantFiled: November 15, 2001Date of Patent: June 27, 2006Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Hirohiko Kimura, Masato Omatsu, Kazuhiro Yamamoto, Ryuji Miyamoto
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Patent number: 7041666Abstract: Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(?CH2)CH3, —C?C—CH3, —CH?C(CH3)2, or —CH?CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.Type: GrantFiled: November 26, 2002Date of Patent: May 9, 2006Assignee: Schering CorporationInventors: Julius J. Matasi, John P. Caldwell, Deen Tulshian, Lisa S. Silverman, Bernard R. Neustadt
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Patent number: 7041667Abstract: Compounds of Formula 1 [Region ?]—[Region ?]—[Region ?]—[Region ?]??(1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: May 9, 2006Assignee: Pfizer, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 7038047Abstract: Substituted 6-(2-methoxy-phenyl)-triazolopyrimidines of formula I in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, or alkadienyl, haloalkyl, haloalkenyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted; L1, L2 independently denote hydrogen or halogen, provided that at least one from L1 or L2 is halogen; X is halogen, cyano, alkyl, alkoxy, haloalkoxy or alkenyloxy; processes for their preparation, compositiType: GrantFiled: July 8, 2002Date of Patent: May 2, 2006Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Michael Rack, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 6992188Abstract: Corticotropin-releasing factor (CRF) antagonists having the formula wherein the dashed lines, A, B, D E, F, Z, G, R3, and R5 having the definitions set forth in the specification pharmaceutical compositions containing them.Type: GrantFiled: December 6, 1996Date of Patent: January 31, 2006Assignee: Pfizer, Inc.Inventor: Yuhpyng L. Chen
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Patent number: 6921762Abstract: Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-?, IL-1?, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: November 15, 2002Date of Patent: July 26, 2005Assignee: Amgen Inc.Inventors: Guolin Cai, Jennifer N. Chau, Celia Dominguez, Yuelie Lu, Gilbert M. Rishton
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Patent number: 6911443Abstract: A compound of the formula (I) in which R1 is —OR11, —SR11, —SOR11, —SO2R11, —NHR11, or —NR12R13 , and R11, R12, and R13 are as defined broadly in the text. R2 is H, C1-C6alkyl, carbamoyl, or an ester group. R3 is thienyl, pyridyl optionally substituted by halogen or C1-C6alkoxy; naphthyl optionally substituted by C1-C6alkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.Type: GrantFiled: April 17, 2001Date of Patent: June 28, 2005Assignee: Bayer AktiengesellschaftInventors: Takeshi Yura, Arnel B. Concepcion, Gyoonhee Han, Makiko Marumo, Hiroko Yoshino, Norihiro Kawamura, Toshio Kokubo, Hiroshi Komura, Yingfu Li, Timothy B. Lowinger, Muneto Mogi, Noriyuki Yamamoto, Nagahiro Yoshida, Scott Miller, Margaret A. Popp, Aniko M. Redmann, Martha E. Rodriguez, William J. Scott, Ming Wang
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Patent number: 6900217Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, T, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.Type: GrantFiled: May 30, 2002Date of Patent: May 31, 2005Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 6875772Abstract: Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.Type: GrantFiled: November 26, 2002Date of Patent: April 5, 2005Assignee: Schering CorporationInventors: Bernard R. Neustadt, Hong Liu
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Patent number: 6855718Abstract: A 7-(R)-Aminotriazolopyrimidines of formula I where the substituents and index are as defined below: R1 is hydrogen or methyl; R2 is methyl; R3 is C2-C10-alkyl, C1-C4-alkoxymethyl, C3-C10-cycloalkyl; Y is halogen, cyano, C1-C4-alkyl or C1-C4-alkoxy; where * is a center of chirality in the R configuration, processes for their preparation, compositions comprising them and their use for controlling harmful fungi.Type: GrantFiled: November 9, 2001Date of Patent: February 15, 2005Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Klaus Ditrich, Hubert Sauter, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 6828326Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Patent number: 6806268Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula IA and or IB:Type: GrantFiled: May 30, 2002Date of Patent: October 19, 2004Assignee: Alteon, Inc.Inventor: Martin Gall
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Publication number: 20040176398Abstract: Novel triazolopyrimidines of the formula 1Type: ApplicationFiled: March 26, 2004Publication date: September 9, 2004Inventors: Olaf Gebauer, Jorg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Kruger, Ralf Dunkel, Arnd Voerste
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Publication number: 20040167136Abstract: Substituted 6-(2-methoxy-phenyl)-triazolopyrimidines of formula I 1Type: ApplicationFiled: January 12, 2004Publication date: August 26, 2004Inventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Frank Schieweck, Michael Rack, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20040162286Abstract: Substituted 6-(2-tolyl)-triazolopyrimidines of formula (I) in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, or alkadienyl, haloalkyl, haloalkenyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted; R3 is halogen, cyano, alkyl, alkoxy, haloalkyl, or C(═O)A, wherein A is hydrogen, hydroxy, alkyl, amino, or mono- or dialkyl-amino; n is an integer from 1 to 4; and X is halogen, cyano, alkyl, alkoxy, haloalkoxy or alkenylType: ApplicationFiled: January 12, 2004Publication date: August 19, 2004Inventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheim, Ingo Rose, Peter Schafer, Frank Schieweck, Michael Rack, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20040162428Abstract: 6-(2,6-Difluoro-phenyl)-triazolopyrimidines of formula (I), in which R1 and R2 independently denote hydrogen or Alkyl, Alkyl, Alkenyl, Alkynyl, or alkadienyl, cycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or oxygen atom. Or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or xygen atom where R1 and R2 radicals may be unsubstituted or substituted as defined in the description, or R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered hetericyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulphur or oxygen atom, which may be substituted; X is halogen, cyano, alkoxy, haloalkoxy or alkenyloxy; Processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.Type: ApplicationFiled: January 12, 2004Publication date: August 19, 2004Inventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andrea Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20040157863Abstract: Novel triazolopyrimidines of the formula 1Type: ApplicationFiled: April 7, 2004Publication date: August 12, 2004Inventors: Olaf Gebauer, Jorg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Kruger, Ralf Dunkel, Arnd Voerste, Ronald Ebbert, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck, Yoshinori Kitagawa
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Publication number: 20040142943Abstract: Novel triazolopyrimidines of the formula 1Type: ApplicationFiled: March 24, 2004Publication date: July 22, 2004Inventors: Olaf Gebauer, Jorg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Kruger, Fritz Maurer, Ralf Dunkel, Arnd Voerste, Ronald Ebbert, Ulrike Wachendorff-Neumann, Yoshinori Kitagawa, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Publication number: 20040110751Abstract: 6-(2-Chloro-6-fluoro-phenyl)-triazolopyrimidines of formula (I), in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, alkadienyl, or haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or partially or fully halogenated or may be substituted as defined in the description. R1 and R2 together with the interjacent nitrogen atom represent a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted; X is cyano, alkoxy, haloalkoxy or alkenyloxy; processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.Type: ApplicationFiled: October 8, 2003Publication date: June 10, 2004Inventors: Jordi Tormo i Blasco, Hubert Sauter, Bernd Muller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 6747033Abstract: Compounds of formula I in which R1 is alkyl, alkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, trihydrocarbylsilyl, formyl, alkanoyl or alkoxycarbonyl group being attached either to the nitrogen in the 3- or 4-position; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic groups containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R3 is phenyl, cycloalkyl or 5- or 6-membered heteroaryl containing besides carbon atoms one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R4 is halogen, amino, alkoxy, haloalkoxy, alkylamino or dialkylamino; wherein the bent line indicates that the double Bond may be located between the 3- and 9-position or the 4- and 9-Position; and the zigzag line indicates that the groups connected may have the (E)- or (Z)-configuration; RType: GrantFiled: June 12, 2001Date of Patent: June 8, 2004Assignee: BASF AktiengesellschaftInventor: Waldemar Pfrengle
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Patent number: 6740654Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the saltType: GrantFiled: July 5, 2001Date of Patent: May 25, 2004Assignee: Celltech R & D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20040097522Abstract: Novel triazolopyrimidines of the formula 1Type: ApplicationFiled: November 17, 2003Publication date: May 20, 2004Inventors: Olaf Gebauer, Hans-Ludwig Elbe, Marielouise Schneider, Albrecht Marhold, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Arnd Voerste, Yoshinori Kitagawa, Ulrich Heinemann, Petra Hilgers, Axel Pleschke
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Publication number: 20040043991Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: August 5, 2003Publication date: March 4, 2004Inventors: Joseph Armand Picard, Michael William Wilson
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Patent number: 6699874Abstract: Fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of (a) at least one azolopyrimidine of formula I in which R1, R2, L1, L2 and L3 have the meaning given in claim 1; and (b) at least one fungicidal active ingredient selected from benomyl, carboxin, captan, chlorothalonil, copper oxychloride, cyprodinil, dimethomorph, dithianon, dodine, famoxadone, fenhexamid, fenpiclonil, fenpropimorph, fluazinam, mancozeb, metalaxyl, pyrimethanil, quinoxifen, sulfur, triforine, vinclozolin, a fungicidal triazole derivative, and a synthetic strobilurine derivative. The invention also provides a method of controlling the growth of phytopathogenic fungi at a locus by applying synergistically effective amounts of at least one azolopyrimidine of formula I and at least one fungicidal active ingredient (b) to the locus.Type: GrantFiled: December 10, 2002Date of Patent: March 2, 2004Assignee: BASF AktiengesellschaftInventors: Henry Van Tuyl Cotter, Leslie May, Gunter Reichert, Ewald Sieverding
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Publication number: 20030216411Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: January 28, 2003Publication date: November 20, 2003Applicant: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Timothy D. Gross, Ying Hing Gao, Patrick J. Connors, Zhiqiang Guo, Chen Chen
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Publication number: 20030212080Abstract: This invention relates to compounds having the structural formula I 1Type: ApplicationFiled: November 26, 2002Publication date: November 13, 2003Applicant: Schering CorporationInventors: Julius J. Matasi, John P. Caldwell, Deen Tulshian, Lisa S. Silverman, Bernard R. Neustadt
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Patent number: 6645918Abstract: N-(Triazolo[1,5-a]pyrimidinyl)thiophenesulfonamide compounds were prepared from appropriately substituted 2-amino[1,2,4]triazolo[1,5-a]pyrimidine compounds and appropriately substituted thiophenesulfonyl chloride compounds. The compounds were found to be useful as herbicides.Type: GrantFiled: December 19, 2002Date of Patent: November 11, 2003Assignee: Dow AgroSciences LLCInventors: Kim Eric Arndt, Timothy Calvin Johnson, David George Ouse
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Patent number: 6642229Abstract: A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.Type: GrantFiled: November 22, 2002Date of Patent: November 4, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
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Publication number: 20030199393Abstract: N-(Triazolo[1,5-a]pyrimidinyl)thiophene-sulfonamide compounds were prepared from appropriately substituted 2-amino[1,2,4]triazolo[1,5-a]pyrimidine compounds and appropriately substituted thiophene-sulfonyl chloride compounds. The compounds were found to be useful as herbicides.Type: ApplicationFiled: December 19, 2002Publication date: October 23, 2003Inventors: Kim Eric Arndt, Timothy Calvin Johnson, David George Ouse
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Patent number: 6635647Abstract: The invention provides compounds of formula (I) wherein A, B and R are as defined herein and the preparation thereof. The compounds of formula (I) are useful as somatostatin antagonists.Type: GrantFiled: September 18, 2002Date of Patent: October 21, 2003Assignee: Novartis AGInventor: Thomas J. Troxler
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Publication number: 20030195221Abstract: Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: November 15, 2002Publication date: October 16, 2003Inventors: Guolin Cai, Jennifer N. Chau, Celia Dominguez, Yuelie Lu, Gilbert M. Rishton
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Publication number: 20030191130Abstract: Compounds having the structural formula I 1Type: ApplicationFiled: November 26, 2002Publication date: October 9, 2003Applicant: Schering CorporationInventors: Bernard R. Neustadt, Hong Liu
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Patent number: 6613773Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.Type: GrantFiled: March 5, 2002Date of Patent: September 2, 2003Assignee: Syngenta LimitedInventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
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Publication number: 20030158197Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.Type: ApplicationFiled: November 8, 2002Publication date: August 21, 2003Applicant: NEUROGEN CORPORATIONInventors: Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 6586430Abstract: Compounds of Formula 1 [Region &agr;]-[Region &bgr;]-[Region &ggr;]-[Region &dgr;] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: July 1, 2003Assignee: Pfizer Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Publication number: 20030120072Abstract: 1 The invention provides compounds of formula (I), wherein A, B and R are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as somatostatin receptor antagonists.Type: ApplicationFiled: September 18, 2002Publication date: June 26, 2003Inventor: Thomas J. Troxler
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Patent number: 6570014Abstract: A process for preparing triazolopyrimidine derivatives of the formula (I): wherein R1 represents a hydrogen or an alkyl radical of one to ten carbon atoms, or a cycloalkyl radical of three to six carbon atoms, or an alkenyl radical of up to four carbon atoms; R2 represents a hydrogen, a halogen atom, a hydroxyalkyl or alkyl radical of one to ten carbon atoms; R3 represents a hydrogen, a hydroxyalkyl or alkyl radical of one to four carbon atoms; by rapidly preparing diamino-1,2,4-triazole which is reacted with an aldehyde to form an imide which is reacted with an &agr;,&bgr;-unsaturated acid derivative, the reaction product of which is hydrolyzed in the presence of an acid to produce the triazolopyrimidine derivatives of formula (I). The compounds of the formula (I) are capable of preventing bronchospasm.Type: GrantFiled: April 30, 2002Date of Patent: May 27, 2003Assignee: Sinon CorporationInventors: Chien-Hsing Chen, Chun-Lin Yeh, Yu-Hwa Chuang
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Patent number: 6559151Abstract: 6-(2-Trifluoromethyl-phenyl)-triazolopyrimidines of formula I in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, alkadienyl, or haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or substituted as defined in the specification; or R1 and R2 together with the interjacent nitrogen atom represents a 5- or 6-membered heterocyclic ring, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which may be substituted as defined in the specification; R3 is hydrogen, halogen, alkyl, alkoxy and haloalkyl; and X is halogen; processes and intermediates for preparing these compounds, compositions comprising them aType: GrantFiled: December 12, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Klaus Jüergen Pees, Frank Schieweck, Jordi Tormo I Blasco, Hubert Sauter, Oliver Cullman, Bernd Müller, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Eberhard Ammermann, Siegried Strathmann, Gisela Lorenz, Rheinhard Stierl
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Publication number: 20030083328Abstract: Compound of formula I 1Type: ApplicationFiled: June 12, 2001Publication date: May 1, 2003Inventor: Waldemar Pfrengle
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Patent number: 6551761Abstract: This invention relates to &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetraaryl- or triarylalkylborate salts which can be photochemically converted into amines, imines or amidines as well as to a process for their preparation. This invention also relates to base-polymerisable or crosslinkable compositions comprising these &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetra- or triarylalkylborate salts, to a process for carrying out photochemically induced, base-catalysed reactions as well as to their use as photoinitiators for base-catalysed reactions.Type: GrantFiled: September 7, 2000Date of Patent: April 22, 2003Assignee: Ciba Specialty Chemical CorporationInventors: Véronique Hall-Goulle, Sean Colm Turner, Allan Francis Cunningham
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Patent number: 6545000Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine compounds represented by formula (I): wherein na and nb independently represent an integer of 0 to 4 and Q represents a hydrogen atom or 3,4-dimethoxybenzyl, or salts thereof exhibit activity as adenosine A2A receptor antagonists.Type: GrantFiled: March 22, 2001Date of Patent: April 8, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Junichi Shimada, Hironori Imma, Naoto Osakada, Shizuo Shiozaki, Tomoyuki Kanda, Yoshihisa Kuwana
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Patent number: 6537998Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: October 16, 2000Date of Patent: March 25, 2003Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Timothy D. Gross, Yinghong Gao, Patrick J. Connors, Jr., Zhiqiang Guo, Chen Chen
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Publication number: 20030055069Abstract: The novel compounds of formula I: 1Type: ApplicationFiled: April 23, 2001Publication date: March 20, 2003Applicant: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Guenter Krummel, Henry Van Tuyl Cotter, Guido Albert, Annerose Rehnig, Leslie May, Waldemar Pfrengle